Methods and Compositions for the Treatment of Lupus Using Clofarabine

a technology of lupus and compositions, applied in the field of methods and compositions for the treatment of lupus using clofarabine, can solve the problems of suppressing the immune system's ability to fight infection, worsening the course of the disease, and reducing the effect of the spread or worsening of the diseas

Inactive Publication Date: 2009-12-03
WOOD CHRISTOPHER B +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0021]As used herein, a “therapeutically effective amount” refers to that amount of the compound of the invention or other active ingredient sufficient to provide a therapeutic benefit in the treatment or management of the disease or to delay or minimize symptoms associated with the disease. Further, a therapeutically effective amount with respect to a compound of the invention means that amount of therapeutic agent alone, or in combination with other therapies, that provides a therapeutic benefit in the treatment or management of the disease. Used in connection with an amount of a compound of the invention, the term can encompass an amount that improves overall therapy, reduces or avoids symptoms or causes of disease, or enhances the therapeutic efficacy of or synergies with another therapeutic agent.
[0028]As used herein, the terms “treat”, “treating” and “treatment” refer to the eradication or amelioration of the disease or symptoms associated with the disease. In certain embodiments, such terms refer to minimizing the spread or worsening of the disease resulting from the administration of one or more prophylactic or therapeutic agents to a subject with such a disease.

Problems solved by technology

Autoimmune disorders, however, cause the immune system to mistakenly attack the cells, tissues, and organs of a patient's own body.
Sunlight not only acts as a trigger for lupus but can worsen the course of the disease.
Unfortunately, these medications also suppress the ability of the immune system to fight infection and have other potentially serious side effects.
However, all of the potential uses for clofarabine have thus far remained unexplored or undeveloped.

Method used

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  • Methods and Compositions for the Treatment of Lupus Using Clofarabine

Examples

Experimental program
Comparison scheme
Effect test

example 1

5.1 Example 1

Parenteral Dosage Formulation

[0105]Clofarabine, 9.86 g, is wetted / partially dissolved with 600 mL of a 9:1 mixture of tertiary butanol and Water for Injection USP which is pre-cooled to 5° C. Once the drug powder is completely wetted, dissolution is completed by the addition of 600 mL of a 1:9 mixture of tertiary butanol and Water for Injection and 766 mL of a 1:1 mixture of tertiary butanol and Water for Injection which likewise is pre-cooled to 5° C. thereby making the final solution a 1:1 mixture. The dissolution is carried out under protection from light.

[0106]The solution formed above is promptly lyophilized in a Virtis INOTOP lyophilizer at −16° C. under light protectant conditions over a period of 48 hours. The resultant lyophilized product (lyophile) is then further dried at 15° C. under high vacuum for 48 hours. No detectable degradation of the drug is observed during these procedures. The lyophile is packaged under sterile conditions into 30 mL vials, each con...

example 2

5.2 Example 2

25 mg Dosage Capsule

[0108]Table 1 illustrates a batch formulation and a single dose unit formulation containing 25 mg of Clofarabine.

TABLE 1Formulation for 25 mg tabletPercentQuantityQuantityMaterialby Weight(mg / tablet)(kg / batch)Clofarabine 40%25.0020.00Microcrystalline53.5% 33.4426.75Cellulose, NFPluronic F-684.0%2.502.00SurfactantCroscarmellose2.0%1.251.00Sodium Type A, NFMagnesium Stearate, NF0.5%0.31250.25Total100.0% 62.50 mg50.00 kg

[0109]The microcrystalline cellulose, croscarmellose sodium, and Clofarabine components are passed through a #30 mesh screen (about 430μ to about 655μ). The Pluronic F-68® (manufactured by JRH Biosciences, Inc. of Lenexa, Kans.) surfactant is passed through a #20 mesh screen (about 457μ to about 1041μ). The Pluronic F-68® surfactant and 0.5 kgs of croscarmellose sodium are loaded into a 16 qt. twin shell tumble blender and are mixed for about 5 minutes. The mix is then transferred to a 3 cubic foot twin shell tumble blender where the mic...

example 4

5.4 Example 4

200 mg Dosage Capsule

[0113]Table 3 illustrates a batch formulation and single dosage formulation for a 200 mg Clofarabine single dose unit, i.e., about 40 percent by weight.

TABLE 3Formulation for 200 mg capsulePercentQuantityQuantityMaterialBy Weight(mg / tablet)(kg / batch)Clofarabine40.0%200mg16.80 kgPregelatinized Corn9.5%297.5mg24.99 kgStarch, NF5Magnesium Stearate0.5%2.5mg 0.21 kgTotal100.0%500mg42.00 kg

[0114]The pregelatinized corn starch (SPRESS B-820) and 3-[2-(3′-methyl-biphen-4-yloxy)-acetylamino]-benzoic acid components are passed through a 710 μm screen and then are loaded into a Diffusion Mixer with a baffle insert and blended for 15 minutes. The magnesium stearate is passed through a 210 μm screen and is added to the Diffusion Mixer. The blend is then encapsulated in a size #0 capsule, 500 mg per capsule (8400 capsule batch size) using a Dosator type capsule filling machine.

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Abstract

This invention relates to methods of treating or preventing lupus comprising the administration of clofarabine or a pharmaceutically acceptable salt, hydrate, solvate or clathrate thereof to a patient in need of such treatment. The invention further relates to methods of treating or preventing lupus comprising the administration of clofarabine or a pharmaceutically acceptable salt, hydrate, solvate or clathrate thereof and an additional therapeutic agent to a patient in need of such treatment.

Description

[0001]This application is a divisional of U.S. application Ser. No. 10 / 529,520 filed Nov. 16, 2005, now abandoned, which is a U.S. national stage application filed under 35 U.S.C. § 371 of International Application No. PCT / US03 / 30407 filed Sep. 25, 2003, which claims the benefit of priority under 35 U.S.C. § 119(e) of U.S. provisional Application No. 60 / 414,685 filed Sep. 27, 2002, the contents of all of which are hereby incorporated herein by their entirety for all purposes.1. FIELD OF THE INVENTION[0002]This invention relates to pharmaceutical compositions, dosage forms and dosage regimens utilizing clofarabine. This invention also relates to methods of treating lupus, and to methods for dosing clofarabine, each of these methods also encompasses reducing or avoiding undesired effects associated with conventional treatment of lupus.2. BACKGROUND OF THE INVENTION2.1 Lupus[0003]The immune system is a complicated network of cells and cell components that defend the body and eliminate ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K38/21A61K31/7076A61P37/06A61KA61K31/34A61K31/52A61P37/00
CPCA61K31/7076A61K31/34A61P37/00A61P37/06
Inventor WOOD, CHRISTOPHER B.SMITH, STUART WILLIAM GORDON
Owner WOOD CHRISTOPHER B
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